Prednizol

General characteristics. Structure:

Active ingredient: 30 mg of Prednisolonum (in the form of phosphate sodium).

Excipients: dinatrium эдетат, sodium hydrophosphate anhydrous, dihydrophosphate sodium a dihydrate, propylene glycol, water for and.

Pharmacological properties:

Pharmacodynamics. Prednizol - synthetic glucocorticoid drug, the dehydrogenated hydrocortisone analog. Has an antiinflammatory, antiallergic, immunodepressive effect, increases sensitivity of beta adrenoceptors to endogenous catecholamines.

Interacts with specific cytoplasmatic receptors (receptors for glucocorticosteroids (GKS) are in all fabrics, especially their is a lot of in a liver) with formation of the complex inducing formation of proteins (including the enzymes regulating the vital processes in cells.)

Protein metabolism: reduces amount of globulins in plasma, increases synthesis of albumine in a liver and kidneys (with increase in coefficient albumine/globulin), reduces synthesis and strengthens a protein catabolism in muscular tissue.

Lipidic exchange: increases synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat happens preferential in the field of a shoulder girdle, the person, a stomach), leads to development of a hypercholesterolemia.

Carbohydrate metabolism: increases absorption of carbohydrates from digestive tract; increases activity of glyukozo-6-phosphatase (increase in intake of glucose from a liver in blood); increases activity of a fosfoenolpiruvatkarboksilaza and synthesis of aminotransferases (activation of a gluconeogenesis); promotes development of a hyperglycemia.

Water элетролитный exchange: Na + and water in an organism detains, stimulates removal of K+ (mineralokortikoidny activity), reduces absorption of Sa2 + from digestive tract, reduces a mineralization of a bone tissue.

The antiinflammatory effect is connected with release oppression by eosinophils and mast cells of mediators of an inflammation; induction of formation of lipokortin and reduction of quantity of the mast cells producing hyaluronic acid; with reduction of permeability of capillaries; stabilization of cellular membranes (especially lizosomalny) and membranes of organellas. Affects all stages of inflammatory process: inhibits synthesis of prostaglandins at the level of arachidonic acid (липокортин oppresses A2 phospholipase, suppresses a liberation of arachidonic acid and inhibits biosynthesis of endoperoxides, the leukotrienes promoting processes of an inflammation, an allergy, etc.), synthesis of "pro-inflammatory cytokines" (Interlaken 1, a tumor necrosis factor an alpha, etc.); increases resistance of a cellular membrane to action of various disturbing factors.

The immunodepressive effect is caused by the caused involution of an adenoid tissue, oppression of proliferation of lymphocytes (especially T lymphocytes), suppression of migration of V-cells and interactions of T - and V-lymphocytes, braking of release of cytokines (interleykina-1, 2; gamma interferon) from lymphocytes and macrophages and decrease in antibody formation.

The antiallergic effect develops as a result of decrease in synthesis and secretion of mediators of an allergy, braking of release from sensitized mast cells and basophiles of a histamine, etc. biologically active agents, reduction of number of the circulating basophiles, T - and V-lymphocytes, mast cells; suppression of development of adenoid and connecting tissue, decrease in sensitivity of effector cells to mediators of an allergy, oppression of antibodyformation, change of an immune response of an organism.

At obstructive respiratory diseases action is caused, mainly, by braking of inflammatory processes, the prevention or reduction of expressiveness of hypostasis of mucous membranes, decrease in eosinophilic infiltration of a submucosal layer of an epithelium of bronchial tubes and adjournment in mucous bronchial tubes of the circulating cell-bound immune complexes, and also braking of an erozirovaniye and desquamation mucous. Increases sensitivity of beta adrenoceptors of bronchial tubes of small and average caliber to endogenous catecholamines and exogenous sympathomimetics, reduces viscosity of slime due to reduction of its products.

Suppresses synthesis and secretion of AKTG and for the second time - synthesis of endogenous GKS. Slows down connective tissue reactions during inflammatory process and reduces a possibility of formation of cicatricial fabric.

Pharmacokinetics. To 90% of drug contacts proteins of plasma: transcortinum (kortizolsvyazyvayushchy globulin) and albumine. Prednisolonum is metabolized in a liver, partially in kidneys and other fabrics, generally by conjugation with glucuronic and sulfuric acids. Metabolites are inactive. It is removed with bile and with urine by glomerular filtering and for 80-90% it reabsorbirutsya by tubules. 20% of a dose are removed by kidneys in not changed look. T1/2 from plasma after intravenous administration 2-3 hours.

Indications to use:

Prednizol apply to the emergency therapy at the states demanding bystry increase in concentration of glucocorticosteroids in an organism:

— depressed cases (burn, traumatic, operational, toxic, cardiogenic) - at inefficiency of vasoconstrictors, plasma substituting drugs and other symptomatic therapy;

— allergic reactions (acute severe forms), hemotransfusionic shock, acute anaphylaxis, anaphylactoid reactions;

— wet brain (including against the background of a tumor of a brain or connected with surgical intervention, radiation therapy or an injury of the head);

— bronchial asthma (severe form), asthmatic status;

— general diseases of connecting fabric (system lupus erythematosus, pseudorheumatism);

— acute adrenal insufficiency;

— thyrocardiac crisis;

— acute hepatitis, hepatic coma;

— reduction of the inflammatory phenomena and the prevention of cicatricial narrowings (at poisoning with the cauterizing liquids).

Route of administration and doses:

The dose of drug and duration of treatment is established by the doctor individually depending on indications and disease severity. Prednizol enter intravenously (kapelno or struyno) or intramusculary. Intravenously the drug is usually administered at first struyno, then kapelno.

At acute insufficiency of adrenal glands the single dose of drug makes 100-200 mg, daily 300-400 mg.

At heavy allergic reactions Prednizol enter in a daily dose 100-200 mg within 3-16 days.

At bronchial asthma the drug is administered depending on disease severity and efficiency of complex treatment from 75 to 675 mg on a course of treatment from 3 to 16 days; in hard cases the dose can be raised to 1400 mg on a course of treatment and more with a gradual dose decline.

At the asthmatic status Prednizol enter in a dose 500-1200 mg a day with the subsequent decrease to 300 mg a day and transition to maintenance doses.

At thyrocardiac crisis enter on 100 mg of drug in a daily dose 200-300 mg; if necessary the daily dose can be increased to 1000 mg. Duration of introduction depends on therapeutic effect, usually up to 6 days.

At shock, resistant to standard therapy, Prednizol at the beginning of therapy usually enter struyno then pass to drop introduction. If within 10-20 minutes arterial pressure does not increase, povtoryayut.struyny administration of drug. After removal from a depressed case continue drop introduction before stabilization of arterial pressure. The single dose makes 50-150 mg (in hard cases - to 400 mg). Repeatedly the drug is administered in 3-4 hours. The daily dose can make 300-1200 mg (with the subsequent dose decline).

At acute hepatonephric insufficiency (at acute poisonings, in the postoperative and puerperal periods, etc.), Prednizol enter 25-75 mg a day; in the presence of indications the daily dose can be increased to 300-1500 mg a day and above.

At a pseudorheumatism and a system lupus erythematosus Prednizol enter in addition to system administration of drug in a dose 75 - 125 mg a day no more than 7-10 days.

At an acute hepatitis Prednizol enter 75-100 mg a day within 7-10 days.

At poisonings with the cauterizing liquids with burns of a digestive tract and upper respiratory tracts Prednizol appoint in a dose 75-400 mg a day within 3-18 days.

At impossibility of intravenous administration, Prednizol enter intramusculary in the same doses. After stopping of an acute state appoint inside Prednizol in tablets, with the subsequent gradual reduction of a dose. At long administration of drug the daily dose should be reduced gradually. Long therapy cannot be stopped suddenly!

Features of use:

Use at pregnancy and feeding by a breast. At pregnancy (especially in the I trimester) apply only according to vital indications.

As glucocorticosteroids get into breast milk, in case of need uses of drug during breastfeeding, feeding by a breast is recommended to be stopped.

Use at abnormal liver functions. To apply with care at a heavy chronic liver failure.

Use at renal failures. To apply with care at a heavy chronic renal failure, a nefrourolitiaza.

Use for children. At children in a growth period of GKS have to be applied only according to absolute indications and under especially careful observation of the attending physician.

Special instructions. During treatment by Prednizol (especially long) observation of the oculist, control of the ABP, a condition of water and electrolytic balance, and also a picture of peripheral blood and level of glucose of blood is necessary.

For the purpose of reduction of by-effects it is possible to appoint antacids, and also to increase receipt of K+ in an organism (a diet, potassium drugs). Food has to be protein-rich, vitamins, with restriction of content of fats, carbohydrates and table salt.

Effect of drug amplifies at patients with a hypothyroidism and cirrhosis. Drug can increase the existing emotional instability or psychotic disturbances. At the instruction in the anamnesis Prednizol in high doses appoint to psychoses under strict control of the doctor.

With care it is necessary to apply at an acute and subacute myocardial infarction - distribution of the center of a necrosis, delay of formation of cicatricial fabric and a rupture of a cardiac muscle is possible.

In stressful situations during the supporting treatment (for example, surgeries, an injury or infectious diseases) it is necessary to carry out dose adjustment of drug in connection with increase in need for glucocorticosteroids.

At sudden cancellation, especially in case of the previous use of high doses, development of a syndrome of "cancellation" (anorexia, nausea, block, generalized musculoskeletal pains, the general weakness), and also an exacerbation of a disease concerning which Prednizol was appointed is possible.

During treatment by Prednizol it is not necessary to carry out vaccination in connection with decrease in its efficiency (immune response).

Appointing Prednizol at intercurrent infections, septic states and tuberculosis, it is necessary to carry out treatment by antibiotics of bactericidal action at the same time.

At children during prolonged treatment by Prednizol careful observation of dynamics of growth and development is necessary. To children who during treatment were in contact with patients with measles or chicken pox preventively appoint specific immunoglobulins.

Owing to weak mineralokortikoidny effect for replacement therapy at adrenal insufficiency Prednizol use in a combination from mineralokortikoida.

At patients with a diabetes mellitus it is necessary to control the content of glucose of blood and if necessary to korrigirovat therapy.

Radiological control of bone and joint system (pictures of a backbone, brush) is shown.

Prednizol with latent infectious diseases of kidneys and urinary tract is capable to cause a leukocyturia in patients that can have diagnostic value.

Prednizol increases the maintenance of metabolites of 11-and 17 oxyketocorticosteroids.

Side effects:

Frequency of development and expressiveness of side effects depends on duration of use, size of the used dose and a possibility of observance of a circadian rhythm of appointment of Prednizol.

At Prednizol's use can be noted:

From endocrine system: decrease in tolerance to glucose, a steroid diabetes mellitus or manifestation of a latent diabetes mellitus, oppression of function of adrenal glands, an Icenco-Cushing syndrome (a crescent-shaped face, obesity of pituitary type, a hirsutism, increase in arterial pressure, a dysmenorrhea, an amenorrhea, muscular weakness, striya), a delay of sexual development at children.

From the alimentary system: nausea, vomiting, pancreatitis, steroid stomach ulcer and duodenum, erosive esophagitis, gastrointestinal bleedings and perforation of a wall of digestive tract, increase or loss of appetite, digestion disturbance, meteorism, hiccups. In rare instances - increase in activity of "hepatic" transaminases and an alkaline phosphatase.

From cardiovascular system: arrhythmias, bradycardia (up to a cardiac standstill); development (at predisposed patients) or strengthening of expressiveness of heart failure, change on the ECG characteristic of a hypopotassemia, increase in the ABP, hypercoagulation, fibrinferments. Patients with an acute and subacute myocardial infarction have a distribution of the center of a necrosis, delay of formation of cicatricial fabric that can lead to a rupture of a cardiac muscle.

From a nervous system: delirium, disorientation, euphoria, hallucinations, maniac-depressive psychosis, depression, paranoia, increase in intracranial pressure, nervousness or concern, sleeplessness, dizziness, вертиго, cerebellum pseudoneoplasm, headache, spasms.

From sense bodys: a back subkapsulyarny cataract, increase in intraocular pressure with possible injury of an optic nerve, tendency to development of consecutive bacterial, fungal or viral infections of eyes, trophic changes of a cornea, an exophthalmos, sudden loss of sight (at parenteral administration in the head, a neck, nasal sinks, head skin adjournment of crystals of drug in eye vessels is possible).

From a metabolism: the increased calcium removal, a hypocalcemia, increase in body weight, negative nitrogenous balance (the increased disintegration of proteins), the increased perspiration.

Caused by mineralokortikoidny activity: delay of liquid and sodium (peripheral hypostases), pshernatriyemiya, gipokaliyemichesky syndrome (hypopotassemia, arrhythmia, mialgiya or spasm of muscles, unusual weakness and fatigue).

From a musculoskeletal system: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth), osteoporosis (it is very rare - pathological fractures of bones, an aseptic necrosis of a head humeral and a femur), a rupture of sinews of muscles, a steroid myopathy, decrease in muscle bulk (atrophy).

From integuments and mucous membranes: the slowed-down healing of wounds, petechias, ecchymomas, thinning of skin, hyper - or hypopigmentation, steroid eels, striya, tendency to development of a pyoderma and candidiases.

Allergic reactions: skin rash, itch, acute anaphylaxis, local allergic reactions.

Local at parenteral administration: burning, numbness, pain, a pricking in an injection site, an infection in an injection site, is rare - a necrosis of surrounding fabrics, formation of hems in the place of an injection; an atrophy of skin and hypodermic cellulose at introduction in oil (introduction to a deltoid muscle is especially dangerous).

Others: development or an exacerbation of infections (emergence of this side effect is promoted jointly by the applied immunodepressants and vaccination), a leukocyturia, a syndrome of "cancellation".

Interaction with other medicines:

Pharmaceutical incompatibility of Prednizol with other intravenously administered drugs is possible - he is recommended to be entered separately from other drugs (in/in bolyusno, or through other dropper as the second solution). When mixing solution of Prednizol with heparin the deposit is formed.

Co-administration of Prednizol with:

— inductors of "hepatic" microsomal enzymes (phenobarbital, rifampicin, Phenytoinum, theophylline, ephedrine) leads to decrease in its concentration;

— diuretics (especially "thiazide" and inhibitors of a karboangidraza) and Amphotericinum In - can lead to strengthening of removal from an organism of K+ and increase in risk of development of heart failure;

— with natriysoderzhashchy drugs - to development of hypostases and increase in arterial pressure;

— cardiac glycosides - their portability worsens and the probability of development of a ventricular ekstrasitoliya increases (because of the caused hypopotassemia);

— indirect anticoagulants - weakens (strengthens) their action less often (it is required to dose adjustment);

— anticoagulants and trombolitika • the risk of development of bleedings from ulcers in digestive tract increases;

— ethanol and NPVP - the risk of emergence of erosive cankers in a GIT and development of bleedings (in a combination with NPVP at treatment of arthritises the dose decline of glucocorticosteroids because of summation of therapeutic effect is possible) amplifies;

— paracetamol - the risk of development of a hepatotoxic (induction of liver enzymes and formation of a toxic metabolite of paracetamol) increases;

— acetylsalicylic acid - accelerates its removal and reduces concentration in blood (at Prednizol's cancellation the level of salicylates in blood increases and the risk of development of by-effects increases);

— insulin and peroral hypoglycemic drugs, antihypertensives - their efficiency decreases;

— vitamin D - its influence on absorption of Sa2 + in intestines decreases;

— somatotropic hormone - reduces efficiency of the last, and with prazikvantely - its concentration;

— M-holinoblokatorami (including antitistaminny drugs and tricyclic antidepressants) and nitrates - promotes increase in intraocular pressure;

— an isoniazid and meksiletiny - increases their metabolism (especially at "bystry acetylizers") that leads to decrease in their plasma concentration.

Inhibitors of a karboangidraza and "loopback" diuretics can increase risk of development of osteoporosis.

Indometacin, forcing out Prednizol from communication with albumine, increases risk of development of its side effects.

AKTG strengthens Prednizol's action.

Ergocalciferol and parathormone interfere with development of the osteopathy caused by Prednizol.

Cyclosporine and кетоконазол, slowing down Prednizol's metabolism, can increase its toxicity in some cases.

Co-administration of androgens and steroid anabolic drugs with Prednizol promotes development of peripheral hypostases and a hirsutism, appearance of eels.

Are oestrogenic and oral estrogensoderzhashchy contraceptives reduce Prednizol's clearance that can be followed by strengthening of expressiveness of its action.

Mitotanum and other inhibitors of function of bark of adrenal glands can cause need of increase in a dose of Prednizol.

At simultaneous use with live antiviral vaccines and against the background of other types of immunization increases risk of activation of viruses and development of infections.

Antipsychotic means (neuroleptics) and Azathioprinum increase risk of development of a cataract at Prednizol's appointment.

At simultaneous use with anti-thyroid drugs decreases, and with thyroid hormones - Prednizol's clearance increases.

The hypopotassemia caused by Prednizol can increase expressiveness and duration of muscular blockade against the background of muscle relaxants.

Immunodepressants increase risk of development of injections and a lymphoma or other limfoproliferativny disturbances connected with Epstein's virus - Barrel.

Tricyclic antidepressants can increase expressiveness of the depression caused by Prednizol's reception (are not shown for therapy of these side effects).

Contraindications:

— hypersensitivity to Prednisolonum or components of drug.

At children in a growth period of GKS have to be applied only according to absolute indications and under especially careful observation of the attending physician.

With care:

— gastrointestinal diseases - a peptic ulcer of a stomach and duodenum, an esophagitis, gastritis, an acute or latent round ulcer, recently created intestines anastomosis, nonspecific ulcer colitis with threat of perforation or abscessing, a diverticulitis;

— parasitic and infectious diseases of the virus, fungal or bacterial nature (now or recently postponed, including recent contact with the patient) - the herpes simplex surrounding herpes (a viremichesky phase), chicken pox, measles; amebiasis, strongyloidosis; system mycosis; active and latent tuberculosis. Use at serious infectious diseases is admissible only against the background of specific therapy;

— pre-and the postvaccinal period (8 weeks to and 2 weeks after vaccination), lymphadenitis after BTsZh inoculation;

— immunodeficiency (including AIDS or HIV - an infection);

— diseases of cardiovascular system (including recently postponed myocardial infarction - at patients with an acute and subacute myocardial infarction distribution of the center of a necrosis, delay of formation of cicatricial fabric and, thereof, - a rupture of a cardiac muscle), heavy chronic heart failure, arterial hypertension, a lipidemia is possible);

— endocrine diseases - a diabetes mellitus (including disturbance of tolerance to carbohydrates), a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease, obesity (the III-IV Art.);

— heavy chronic renal and/or liver failure, нефроуролитиаз;

— the hypoalbuminemia and states contributing to its emergence;

— system osteoporosis, gravis myasthenia, acute psychosis, poliomyelitis (except for a form of bulbar encephalitis), open and closed-angle glaucoma;

— pregnancy.

Overdose:

Strengthening of the by-effects described above is possible. It is necessary to reduce Prednizol's dose. Treatment - symptomatic.

Storage conditions:

To store at a temperature not above 25 °C in the place protected from light. Not to freeze. To store in the places unavailable to children. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

1 ml - ampoules of dark glass (3) - trays plastic (1) - packs cardboard.
1 ml - ampoules of dark glass (3) - blisters (1) - packs cardboard.
1 ml - ampoules of dark glass (3) - blisters (20) - packs cardboard.
1 ml - ampoules of dark glass (5) - blisters (1) - packs cardboard.
1 ml - ampoules of dark glass (5) - blisters (20) - packs cardboard.